CA3031100A1 - Macrocycle kinase inhibitors - Google Patents
Macrocycle kinase inhibitors Download PDFInfo
- Publication number
- CA3031100A1 CA3031100A1 CA3031100A CA3031100A CA3031100A1 CA 3031100 A1 CA3031100 A1 CA 3031100A1 CA 3031100 A CA3031100 A CA 3031100A CA 3031100 A CA3031100 A CA 3031100A CA 3031100 A1 CA3031100 A1 CA 3031100A1
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- CA
- Canada
- Prior art keywords
- alkyl
- cycloalkyl
- compound
- nhs
- membered heterocycloalkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- 230000004565 tumor cell growth Effects 0.000 description 1
- 230000004614 tumor growth Effects 0.000 description 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
- 230000003827 upregulation Effects 0.000 description 1
- 229940005605 valeric acid Drugs 0.000 description 1
- 229960003862 vemurafenib Drugs 0.000 description 1
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- GDJZZWYLFXAGFH-UHFFFAOYSA-M xylenesulfonate group Chemical group C1(C(C=CC=C1)C)(C)S(=O)(=O)[O-] GDJZZWYLFXAGFH-UHFFFAOYSA-M 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
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- Rheumatology (AREA)
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- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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Application Number | Priority Date | Filing Date | Title |
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US201662367886P | 2016-07-28 | 2016-07-28 | |
US62/367,886 | 2016-07-28 | ||
PCT/US2017/044214 WO2018022911A1 (en) | 2016-07-28 | 2017-07-27 | Macrocycle kinase inhibitors |
Publications (1)
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CA3031100A1 true CA3031100A1 (en) | 2018-02-01 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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CA3031100A Pending CA3031100A1 (en) | 2016-07-28 | 2017-07-27 | Macrocycle kinase inhibitors |
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US (1) | US10689400B2 (ru) |
EP (1) | EP3490564A4 (ru) |
JP (1) | JP2019527230A (ru) |
KR (1) | KR20190034225A (ru) |
CN (1) | CN109715165A (ru) |
AU (1) | AU2017302019A1 (ru) |
BR (1) | BR112019001607A2 (ru) |
CA (1) | CA3031100A1 (ru) |
IL (1) | IL264395A (ru) |
MX (1) | MX2019001125A (ru) |
RU (1) | RU2019105587A (ru) |
SG (1) | SG11201900163PA (ru) |
TW (1) | TW201815799A (ru) |
WO (1) | WO2018022911A1 (ru) |
ZA (1) | ZA201901034B (ru) |
Families Citing this family (20)
Publication number | Priority date | Publication date | Assignee | Title |
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DK3097107T3 (da) | 2014-01-24 | 2019-07-08 | Turning Point Therapeutics Inc | Diaryl-makrocykler som modulatorer for proteinkinaser |
EP3317285B1 (en) | 2015-07-02 | 2021-01-27 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
KR20180033194A (ko) | 2015-07-21 | 2018-04-02 | 티피 테라퓨틱스, 인크. | 키랄 디아릴 매크로사이클 및 이것의 용도 |
CA3031100A1 (en) | 2016-07-28 | 2018-02-01 | Tp Therapeutics, Inc. | Macrocycle kinase inhibitors |
TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
MY201925A (en) | 2017-07-28 | 2024-03-23 | Turning Point Therapeutics Inc | Macrocyclic compounds and uses thereof |
CN109516999B (zh) * | 2017-11-01 | 2021-08-17 | 郑州泰基鸿诺医药股份有限公司 | 用作蛋白质激酶调节剂的化合物及其应用 |
HUE060711T2 (hu) | 2017-12-19 | 2023-04-28 | Turning Point Therapeutics Inc | Makrociklusos vegyületek betegségek kezelésére |
JP2021519297A (ja) | 2018-03-28 | 2021-08-10 | フォチョン・ファーマシューティカルズ・リミテッドFochon Pharmaceuticals, Ltd. | Trkキナーゼ阻害剤としての大環状化合物 |
CA3224945A1 (en) | 2018-07-31 | 2020-02-06 | Loxo Oncology, Inc. | Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide |
EP3870579A4 (en) | 2018-10-22 | 2022-10-19 | Alumis Inc. | TYK2 INHIBITORS AND THEIR USES |
EP3974434A4 (en) * | 2019-05-21 | 2023-11-08 | Zhejiang Hisun Pharmaceutical Co., Ltd. | MACROLIDE DERIVATIVES, PRODUCTION PROCESS AND USE THEREOF |
CN112110938B (zh) * | 2019-06-21 | 2021-11-09 | 成都海博为药业有限公司 | 一种作为蛋白质激酶抑制剂的化合物及其制备方法和用途 |
WO2021027503A1 (zh) * | 2019-08-12 | 2021-02-18 | 罗欣药业(上海)有限公司 | 三环类化合物、其制备方法、中间体及应用 |
KR20230022151A (ko) * | 2020-03-02 | 2023-02-14 | 터닝 포인트 테라퓨틱스, 인크. | 거대고리 화합물의 치료 용도 |
US20230219978A1 (en) * | 2020-06-04 | 2023-07-13 | Scinnohub Pharmaceutical Co., Ltd | Compound having macrocyclic structure and use thereof |
US20240132517A1 (en) * | 2021-02-10 | 2024-04-25 | Goharmony Therapeutics (Shenzhen) Co., Ltd. | Macrocyclic compound, pharmaceutical composition, and use thereof |
CN113354548A (zh) * | 2021-04-12 | 2021-09-07 | 常熟耐素生物材料科技有限公司 | 一种基于六亚甲基四胺的植物多烯酚醛胺环氧固化剂及其制备方法 |
WO2023078267A1 (zh) * | 2021-11-02 | 2023-05-11 | 赛诺哈勃药业(成都)有限公司 | 作为蛋白激酶调节剂的含氨基大环化合物 |
WO2023208244A1 (zh) * | 2022-04-29 | 2023-11-02 | 南京明德新药研发有限公司 | 大环类化合物及其应用 |
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ATE195935T1 (de) | 1993-03-25 | 2000-09-15 | Upjohn Co | Formyl- oder cyano- substituierte indolderivate mit dopaminergischer wirkung |
GB9800569D0 (en) | 1998-01-12 | 1998-03-11 | Glaxo Group Ltd | Heterocyclic compounds |
US7517882B2 (en) * | 2006-09-18 | 2009-04-14 | Polaris Group | Protein kinase inhibitors |
EA201100450A1 (ru) | 2008-09-08 | 2011-10-31 | Мерк Патент Гмбх | Макроциклические пирамидины в качестве ингибиторов протеинкиназы |
ES2464461T3 (es) | 2008-09-22 | 2014-06-02 | Array Biopharma, Inc. | Compuestos de imidazo[1,2B]piridazina sustituidos como inhibidores de la TRK cinasa |
LT3372605T (lt) | 2008-10-22 | 2022-02-10 | Array Biopharma, Inc. | Pakeistieji pirazolo[1,5-a]pirimidino junginiai, kaip trk kinazės inhibitoriai |
CA2740792C (en) | 2008-10-31 | 2016-06-21 | Genentech, Inc. | Pyrazolopyrimidine jak inhibitor compounds and methods |
EP3521291A1 (en) | 2010-05-20 | 2019-08-07 | Array Biopharma, Inc. | Macrocyclic compounds as trk kinase inhibitors |
US8757434B2 (en) * | 2010-07-01 | 2014-06-24 | The Coca-Cola Company | Merchandiser |
UY33597A (es) | 2010-09-09 | 2012-04-30 | Irm Llc | Compuestos y composiciones como inhibidores de la trk |
EP2508607A1 (en) | 2011-04-07 | 2012-10-10 | Helmholtz-Zentrum für Infektionsforschung GmbH | Medicament for liver regeneration and for treatment of liver failure |
AU2012257513B2 (en) * | 2011-05-19 | 2017-05-11 | Fundación Del Sector Público Estatal Centro Nacional De Investigaciones Oncológicas Carlos III (F.S.P. CNIO) | Macrocyclic compounds as protein kinase inhibitors |
WO2013001310A1 (en) | 2011-06-30 | 2013-01-03 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Macrocyclic compounds and their use as cdk8 inhibitors |
WO2013028471A1 (en) | 2011-08-19 | 2013-02-28 | Merck Sharp & Dohme Corp. | Methods and intermediates for preparing macrolactams |
JP6082397B2 (ja) * | 2011-09-30 | 2017-02-15 | イプセン ファルマ ソシエテ パール アクシオン サンプリフィエIpsen Pharma S.A.S. | マクロ環状lrrk2キナーゼ阻害剤 |
AU2012314376B2 (en) | 2011-09-30 | 2017-04-06 | Oncodesign S.A. | Macrocyclic FLT3 kinase inhibitors |
GEP201606560B (en) | 2012-03-06 | 2016-10-25 | Pfizer | Macrocyclic derivatives for the treatment of proliferative diseases |
MX345830B (es) | 2012-03-09 | 2017-02-17 | Lexicon Pharmaceuticals Inc | Compuestos a base de pirazol[1,5-a]pirimidina, composiciones que los comprenden, y metodos para su uso. |
BR112014022271B1 (pt) | 2012-03-09 | 2021-09-21 | Lexicon Pharmaceuticals, Inc | Compostos com base em imidazo[1,2-b]piridazina, composições compreendendo-os, e usos dos mesmos |
GB201205669D0 (en) | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
BR112015022982A2 (pt) * | 2013-03-15 | 2017-07-18 | Oncodesign Sa | inibidores macrocíclicos de rip2 quinase |
CN104513253A (zh) * | 2013-10-01 | 2015-04-15 | 南京波尔泰药业科技有限公司 | 用于治疗增殖性疾病的大环化合物 |
DK3097107T3 (da) | 2014-01-24 | 2019-07-08 | Turning Point Therapeutics Inc | Diaryl-makrocykler som modulatorer for proteinkinaser |
EP3317285B1 (en) * | 2015-07-02 | 2021-01-27 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
RU2765181C2 (ru) | 2015-07-06 | 2022-01-26 | Тёрнинг Поинт Терапьютикс, Инк. | Полиморфная форма диарильного макроцикла |
KR20180033194A (ko) | 2015-07-21 | 2018-04-02 | 티피 테라퓨틱스, 인크. | 키랄 디아릴 매크로사이클 및 이것의 용도 |
CA3031100A1 (en) | 2016-07-28 | 2018-02-01 | Tp Therapeutics, Inc. | Macrocycle kinase inhibitors |
TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
MY201925A (en) | 2017-07-28 | 2024-03-23 | Turning Point Therapeutics Inc | Macrocyclic compounds and uses thereof |
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2017
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- 2017-07-27 BR BR112019001607-4A patent/BR112019001607A2/pt not_active Application Discontinuation
- 2017-07-27 US US16/320,589 patent/US10689400B2/en active Active
- 2017-07-27 KR KR1020197003927A patent/KR20190034225A/ko not_active Application Discontinuation
- 2017-07-27 SG SG11201900163PA patent/SG11201900163PA/en unknown
- 2017-07-27 RU RU2019105587A patent/RU2019105587A/ru not_active Application Discontinuation
- 2017-07-27 TW TW106125249A patent/TW201815799A/zh unknown
- 2017-07-27 WO PCT/US2017/044214 patent/WO2018022911A1/en unknown
- 2017-07-27 AU AU2017302019A patent/AU2017302019A1/en not_active Abandoned
- 2017-07-27 JP JP2019504675A patent/JP2019527230A/ja active Pending
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- 2017-07-27 MX MX2019001125A patent/MX2019001125A/es unknown
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2019
- 2019-01-22 IL IL264395A patent/IL264395A/en unknown
- 2019-02-18 ZA ZA2019/01034A patent/ZA201901034B/en unknown
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ZA201901034B (en) | 2021-06-30 |
US20190169208A1 (en) | 2019-06-06 |
CN109715165A (zh) | 2019-05-03 |
SG11201900163PA (en) | 2019-02-27 |
IL264395A (en) | 2019-02-28 |
WO2018022911A1 (en) | 2018-02-01 |
US10689400B2 (en) | 2020-06-23 |
MX2019001125A (es) | 2019-06-12 |
RU2019105587A3 (ru) | 2020-11-18 |
EP3490564A4 (en) | 2020-02-26 |
RU2019105587A (ru) | 2020-08-28 |
BR112019001607A2 (pt) | 2019-04-30 |
AU2017302019A1 (en) | 2019-02-07 |
TW201815799A (zh) | 2018-05-01 |
JP2019527230A (ja) | 2019-09-26 |
KR20190034225A (ko) | 2019-04-01 |
EP3490564A1 (en) | 2019-06-05 |
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